Faculty of Pharmaceutical Sciences, Tokyo University of Science, Noda, Chiba, Japan.
Org Lett. 2011 Jun 3;13(11):2904-7. doi: 10.1021/ol200889s. Epub 2011 May 11.
Three novel 1-alkyldaphnane-type diterpenes, stelleralides A-C (4-6), and five known compounds were isolated from the roots of Stellera chamaejasme L. The structures of 4-6 were elucidated by extensive spectroscopic analyses. Several isolated compounds showed potent anti-HIV activity. Compound 4 showed extremely potent anti-HIV activity (EC(90) 0.40 nM) with the lowest cytotoxicity (IC(50) 4.3 μM) and appears to be a promising compound for development into anti-AIDS clinical trial candidates.
从瑞香狼毒( Stellera chamaejasme L.)的根部分离得到三种新型 1-烷基金雀花烷型二萜类化合物,即stelleralide A-C(4-6),以及五种已知化合物。通过广泛的光谱分析确定了 4-6 的结构。几种分离得到的化合物表现出很强的抗 HIV 活性。化合物 4 表现出极强的抗 HIV 活性(EC900.40 nM),同时细胞毒性最低(IC504.3 μM),似乎是一种很有前途的化合物,可开发为抗艾滋病临床试验候选药物。